In vitro Antifungal Evaluation and Studies on the Mode of Action of Xanthoxyline Derivatives

Summary This study describes the fungistatic effect of xanthoxyline (CAS 90-24-4) and its derivatives against a panel of yeasts, filamentous fungi and dermatophytes, by using the agar dilution method. Results indicated that simple structural modifications led to more potent derivatives, especially i...

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Bibliographic Details
Published in:	Arzneimittel-Forschung Vol. 49; no. 12; pp. 1039 - 1043
Main Authors:	Pinheiro, Taˆnia R, Yunesa, Rosendo A, L´pez, Silvia N, Santecchia, Carina B., Zacchino, Susana AS, Filho, V Cechinel
Format:	Journal Article
Language:	English
Published:	Aulendorf (Germany) Editio Cantor Verlag 01-12-1999 Cantor
Subjects:	Acetophenones - chemical synthesis Acetophenones - pharmacology Antibiotics. Antiinfectious agents. Antiparasitic agents Antifungal agents Antifungal Agents - chemical synthesis Antifungal Agents - pharmacology Arthrodermataceae - drug effects Biological and medical sciences Chemical Phenomena Chemistry, Physical Fungi - drug effects Ketoconazole - pharmacology Medical sciences Microbial Sensitivity Tests Neurospora crassa - drug effects Neurospora crassa - ultrastructure Originalarbeit Pharmacology. Drug treatments Trichophyton - drug effects Yeasts - drug effects Dermatophytes Xanthoxyline derivatives antifungal activity, mode of action, synthesis Antifungal drugs Antifungal agent Drug susceptibility test Pharmacognosy Acetophenone derivatives Plant origin Mechanism of action In vitro Biological activity Medicinal plant
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Summary:	Summary This study describes the fungistatic effect of xanthoxyline (CAS 90-24-4) and its derivatives against a panel of yeasts, filamentous fungi and dermatophytes, by using the agar dilution method. Results indicated that simple structural modifications led to more potent derivatives, especially in relation with dermatophytes. The most active compound tested ( 10 ), which is a benzenesulphonyl derivative, was 12-fold more potent than xanthoxyline itself against Tricho- phyton rubrum. The evaluation of the mode of action with the whole cell Neurospora crassa assay, suggested that some selected compounds may be acting by the inhibition of fungal cell-wall polymers synthesis or assembly.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0004-4172 1616-7066
DOI:	10.1055/s-0031-1300548